ES2734584B2 - ETHAMSILATE FOR THE TREATMENT OF HERPES VIRUS INFECTIONS - Google Patents

Description

DESCRIPTION

ETHAMSILATE FOR THE TREATMENT OF INFECTIONS BY

HERPES VIRUSES

FIELD OF THE INVENTION

The invention describes the use of ethamsylate for the manufacture of a medicament for the treatment of viral infections that employ heparan sulfate for cell penetration, more specifically for the treatment of patients suffering from viral herpes simplex infection that occurs on any mucosal surface. or epithelial like genital herpes and herpetic stromal keratitis, and particularly for the treatment of cold sores.

The use of ethamsylate as a therapeutic agent may be as a pharmaceutically acceptable salt or solvate thereof,

BACKGROUND OF THE INVENTION

Herpes simplex virus 1 (HSV-1) is the cause of a lifelong infection that affects 50-90% of the world population. In addition to causing skin lesions, HSV-1 is the leading cause of blindness as a consequence of recurrent corneal infection (Vet Microbiol 2002, 86:17). The main ocular manifestations of herpetic infection are keratitis, blepharitis, conjunctivitis, uveitis, dry eye and retinitis (Arq Bras Ofhalmol 2013; 17: 129-132). HSV-1 is a neurotropic member of the herpes / alpha virus family. Primary infection typically occurs after inoculation of mucosal epithelial surfaces, using heparan sulfate for cell penetration. During initial infection, virions access sensory nerve fibers and are transported to neural cell bodies in the trigeminal ganglia where HSV-1 establishes a latent infection (J Clin Microbiol 2003, 41:84; Sex Transm Infect 2005; 81: 103). HSV-1 is the leading cause of facial injuries (mouth, lips, and eyes) in humans.

The usual treatment of HSV-1 infections generally depends on a combination of antiviral and anti-inflammatory drugs such as corticosteroids, the latter need to be administered for prolonged periods, a circumstance that can cause unwanted side effects. Furthermore, the massive use of acyclovir and nucleoside analogues has led to the emergence of HSV-1 strains resistant to these drugs. Therefore, there is an urgent need to develop alternative and more effective therapies for the control of HSV-1 infections.

The inventors have surprisingly found that local administration of ethamsylate in viral infections employing heparan sulfate for cell penetration shows clinical benefits, something that also occurs with viral infections localized to mucosa and epitheliums and particularly cold sores.

DESCRIPTION OF THE INVENTION

Local administration of the compound can be in the form of creams, gels, ointments, dispersions, solid sticks, emulsions, and microemulsions that can be formulated according to conventional methods using suitable excipients. The vehicles and solvents that can be used are water, Ringer's solution and isotonic sodium chloride solution.

Generally, the dose required to provide an effective amount of the compound and composition, which can be adjusted by someone with sufficient skill, will vary depending on the extent of the disease and the frequency of treatment.

The main object of the present invention is directed to the treatment or prevention of the disease described in this document. Furthermore, the present invention can be used for the treatment or prevention of cold sores and other viral infections that employ heparan sulfate for cell penetration.

Throughout this document, the following terms, unless otherwise indicated, are understood to have the following meanings.

"Patient" refers to the human being and includes both women and men.

"Treating," "treating," or "treating" refers to the use of the compounds of the invention from prophylactic points of view, to prevent symptoms of the disease, or therapeutic, to improve an existing condition.

"Therapeutic agent" includes any therapeutic agent that can be used to treat or prevent the disease described below. The concept of therapeutic agent includes, but is not limited to, antiviral, anti-inflammatory, and the like compounds. The concept of therapeutic agent includes pharmaceutically acceptable salts.

Except where otherwise indicated, all the technical and scientific elements used in this specification have the meaning commonly understood by a person with average knowledge in the matter to which this invention belongs. When this invention is put into practice, the methods and materials that can be used will be similar or equivalent to those described in this specification.

Throughout the description and its claims, the word "represent" and its variants are not intended to exclude other technical characteristics, additives, components or steps. For those skilled in the art, other objects, advantages and characteristics of the invention can be deduced from the description and practical use of the invention.

EXAMPLE OF THE INVENTION

The following example without being limiting describes the use of the present invention.

Efficacy of ethamsylate in the treatment of cold sores

A 44-year-old woman had a cold sore injury to her right lip corner (Figure 1). After evaluating the different treatment options, the patient chose to treat topically by administration of ethamsylate and signed an informed consent. The patient administered etamsylate (OM Pharma Switzerland) in a 12% glycerin solution three times daily until day 4, after the first day of treatment the patient was pain free and after the fourth day of treatment, the patient was Herpetic lesion had healed without any apparent cosmetic disturbance (Figure 1). The patient did not report recurrent episodes of herpetic lesion in her right lip commissure after several months of treatment. Although the exact mechanism of action of ethamsylate is unknown, we can suggest that this drug works by blocking heparan sulfate and, consequently, prevents the penetration of the virus into the cytoplasm.

EXPLANATION OF THE FIGURES

As a complement to the present description and in order to help the characteristics of the invention to be more easily understood, and according to a personalized practical example, said description is accompanied by a set of images that form an integral part thereof, which by way of illustration and without limitation are presented below.

Figure 1. Shows the effects of ethamsylate in the treatment of cold sores. Appearance of the cold sore lesion prior to treatment by local application of ethamsylate (A), at two days (B) and at four days (C). The red circle indicates the right labial commissure, where the cold sore and its evolution appeared (B) and (C).

Claims (2)

1- The use of ethamsylate or solvate thereof or its salts in any pharmaceutical form, as a therapeutic agent, in the manufacture of a medicine for the treatment of viral infections that use heparan sulfate for cell penetration, characterized in that it is used in Herpes simplex virus infections that occur on mucous and epithelial surfaces such as genital herpes and stromal keratitis. 2.- The use of ethamsylate or solvate thereof or its salts in any pharmaceutical form, as a therapeutic agent, in the manufacture of a medicine for the treatment of viral infections that use heparan sulfate for cell penetration, characterized in that it is in infections Cold sores virus.